Research Topics
Species | Milt TeitlerSummaryAffiliation: Albany Medical College Country: USA Publications
Research Grants
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Publications
Ketanserin and spiperone as templates for novel serotonin 5-HT(2A) antagonistsRichard A Glennon
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA
Curr Top Med Chem 2:539-58. 2002....- Binding of beta-carbolines at 5-HT(2) serotonin receptorsBrian Grella
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298-0540, USA
Bioorg Med Chem Lett 13:4421-5. 2003..A binding profile was obtained for selected beta-carbolines... 
A new approach for studying GPCR dimers: drug-induced inactivation and reactivation to reveal GPCR dimer function in vitro, in primary culture, and in vivoMilt Teitler
Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
Pharmacol Ther 133:205-17. 2012..The data obtained using the 5-HT(7) and 5-HT(2A) receptors are strongly supportive of a GPCR homodimer structure, with little evidence of monomer involvement in the function of these receptors...- Pharmacological analysis of the novel, rapid, and potent inactivation of the human 5-Hydroxytryptamine7 receptor by risperidone, 9-OH-Risperidone, and other inactivating antagonistsJessica A Knight
Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208
Mol Pharmacol 75:374-80. 2009..The rapid, potent inactivation of the receptor-G-protein complex by antagonists implies a constitutive, pre-existing complex between the h5-HT(7) receptor and a G-protein... - Clozapine and other competitive antagonists reactivate risperidone-inactivated h5-HT7 receptors: radioligand binding and functional evidence for GPCR homodimer protomer interactionsMilt Teitler
Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
Psychopharmacology (Berl) 212:687-97. 2010..Although risperidone and 9-OH-risperidone ("inactivating antagonists") completely inactivate the receptor, only 50% of the receptors form a pseudo-irreversible complex with these drugs... - Constitutive activity of G-protein coupled receptors: emphasis on serotonin receptorsMilt Teitler
Center for Neuroscience and Neuropharmacology, Albany Medical College, 47 New Scotland Avenue, Albany, N Y 12208, USA
Curr Top Med Chem 2:529-38. 2002..Studies are presented demonstrating the procedures for producing and characterizing constitutive activated forms of serotonin receptors, including the demonstration of inverse agonist activity of drugs on these receptors... - Stable expression of constitutively activated mutant h5HT6 and h5HT7 serotonin receptors: inverse agonist activity of antipsychotic drugsAnil Purohit
Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
Psychopharmacology (Berl) 179:461-9. 2005.... - Risperidone irreversibly binds to and inactivates the h5-HT7 serotonin receptorCarol Smith
A 136, Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Ave, Albany, NY 12208, USA
Mol Pharmacol 70:1264-70. 2006..At the very least, the possibility that highly prescribed drugs, such as risperidone, are irreversibly antagonizing GPCR function in vivo is noteworthy... - Risperidone-induced inactivation and clozapine-induced reactivation of rat cortical astrocyte 5-hydroxytryptamine₇ receptors: evidence for in situ G protein-coupled receptor homodimer protomer cross-talkCarol Smith
Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Ave, Albany, NY 12208, USA
Mol Pharmacol 79:318-25. 2011..The homodimer structure and protomer-protomer cross-talk offer new avenues of research into receptor dysfunction in disease states and the development of novel drugs... - Toward selective drug development for the human 5-hydroxytryptamine 1E receptor: a comparison of 5-hydroxytryptamine 1E and 1F receptor structure-affinity relationshipsMichael T Klein
Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
J Pharmacol Exp Ther 337:860-7. 2011..The insights generated from this study will inform future drug development and molecular modeling studies for both 5-HT(1E) and 5-HT(1F) receptors... - Human 5-HT7 receptor-induced inactivation of forskolin-stimulated adenylate cyclase by risperidone, 9-OH-risperidone and other "inactivating antagonists"Nicole Toohey
Center for Neuropharmacology and Neuroscience, Albany Medical College, 47 New Scotland Avenue, Albany, NY 12208, USA
Mol Pharmacol 76:552-9. 2009..These drugs may produce innovative approaches to the development of therapeutic drugs... - Creation, expression, and characterization of a constitutively active mutant of the human serotonin 5-HT6 receptorAnil Purohit
Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, New York 12208, USA
Synapse 47:218-24. 2003..The inverse agonist action of clozapine indicates that drugs displaying competitive antagonist activity at native 5-HT(6) receptors may display inverse agonist activity at the constitutively activated form of the receptor... - Guinea pig hippocampal 5-HT(1E) receptors: a tool for selective drug developmentMichael T Klein
Center for Neuropharmacology and Neuroscience, Albany Medical College, Albany, New York 12208, USA
J Neurochem 109:268-74. 2009..Using the guinea pig as an animal model should provide important insights into possible functions of this receptor and the therapeutic potential of selective human 5-HT(1E) drugs... - Binding of tryptamine analogs at h5-HT1E receptors: a structure-affinity investigationMałgorzata Dukat
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA
Bioorg Med Chem 12:2545-52. 2004..This finding was supported using quantitative structure-activity analysis (QSAR) techniques such as comparative molecular field analysis (CoMFA) and the program QsarIS... - Arylguanidine and arylbiguanide binding at 5-HT3 serotonin receptors: a QSAR studyRichard A Glennon
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA
Bioorg Med Chem 11:4449-54. 2003..A broader examination of 35 arylguanidines and arylbiguanides revealed that affinity could be described by molecular polarizability, a Chi index term (8chiP), and the sum of all (-Cl) E-State values (SsCl) in the molecule... - Binding of tetrahydrocarboline derivatives at human 5-HT5A receptorsNantaka Khorana
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, Virginia 23298 0540, USA
J Med Chem 46:3930-7. 2003..Evidence is provided that 5-HT(5A) and 5-HT(2A) receptor affinities probably do not covary and that it might be possible, with continued investigation, to develop analogues with enhanced 5-HT(5A) selectivity... - Conformationally-restricted analogues and partition coefficients of the 5-HT3 serotonin receptor ligands meta-chlorophenylbiguanide (mCPBG) and meta-chlorophenylguanidine (mCPG)Ashraf A Rahman
Department of Medicinal Chemistry, School of Pharmacy, Medical College of Virginia Campus, Virginia Commonwealth University, Richmond, VA 23298-0540, USA
Bioorg Med Chem Lett 13:1119-23. 2003..38). The quinazoline structure may represent a pharmacologically-active conformation of these agents, and the arylbiguanides were found more lipid soluble than their arylguanidine counterparts at physiological pH... - gamma-Carbolines: binding at 5-HT5A serotonin receptorsNantaka Khorana
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA
Bioorg Med Chem 11:717-22. 2003..Although 17 also binds at 5-HT(2) receptors, it serves as a novel lead for the further development of 5-HT(5A) ligands... - Evaluation of isotryptamine derivatives at 5-HT(2) serotonin receptorsJean Chang-Fong
Department of Medicinal Chemistry, School of Pharmacy, Virginia Commonwealth University, Richmond, VA 23298, USA
Bioorg Med Chem Lett 12:155-8. 2002..Detailed re-examination of a compound previously reported to display 100-fold 5-HT(2C) selectivity [i.e., S(+)-5,6-difluoro-alpha-methylisotryptamine] revealed that its selectivity versus 5-HT(2A) receptors was, at best, only 10-fold...
Research Grants
- Novel modulation of serotonin receptorsMilt Teitler; Fiscal Year: 2009..Dysfunctions of these modulating mechanisms may underly the psychopathology of various mental diseases. These studies may lead to the development of novel therapeutics for brain dysfunctions, including schizophrenia and depression. ..
- Novel modulation of serotonin receptorsMilt Teitler; Fiscal Year: 2007..Dysfunctions of these modulating mechanisms may underly the psychopathology of various mental diseases. These studies may lead to the development of novel therapeutics for brain dysfunctions, including schizophrenia and depression. ..
- Human 5HT 1E Serotonin Receptor Drug Development (RMI)Milt Teitler; Fiscal Year: 2005..Selective agonists and antagonists for the 5HT1E receptor should, at the least, provide information on the function of this highly expressed receptor, and may lead to novel therapeutics for brain dysfunction. ..
- CONSTITUTIVELY ACTIVE SEROTONIN RECEPTORSMilt Teitler; Fiscal Year: 2005....
- Molecular Biology of 5HT2A receptor expressing synapsesMilt Teitler; Fiscal Year: 2005....
- CONSTITUTIVELY ACTIVE SEROTONIIN RECEPTORSMilt Teitler; Fiscal Year: 1999....
- Novel modulation of serotonin receptorsMilt Teitler; Fiscal Year: 2010..Dysfunctions of these modulating mechanisms may underly the psychopathology of various mental diseases. These studies may lead to the development of novel therapeutics for brain dysfunctions, including schizophrenia and depression. ..